Therapy for neurological diseases

a neurological disease and therapy technology, applied in the field of neurological diseases, can solve the problems of uncontrolled rate therapy, drug tacrine, uncontrolled dosing of drugs, etc., and achieve the effect of slowing the progression of alzheimer's disease and avoiding the toxic range of tacrin

Inactive Publication Date: 2000-03-14
ENCINAL PHARMA INVESTMENTS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

Another object of the invention is to provide a method for administering tacrine by orally administering tacrine in a known dose per unit time, over an extended time to a patient in need of tacrine therapy, while simulta...

Problems solved by technology

The conventional forms deliver the drug by dose-dumping, and this leads to uneven dosing of drug, to uneven blood levels of the drug characterized by peaks and valleys, and accordingly, this does not provide controlled-rate therapy over an extended period of time.
The drug tacrine, however, possesses a low osmotic pressu...

Method used

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  • Therapy for neurological diseases
  • Therapy for neurological diseases
  • Therapy for neurological diseases

Examples

Experimental program
Comparison scheme
Effect test

example 1

A dosage form is manufactured for orally dispensing tacrine to the gastrointestinal tract of a human patient. The dosage form for dispensing tacrine to the gastrointestinal tract is unexpected, as tacrine has a low osmotic pressure that is substantially equivalent to the normal osmotic pressure of 8 plus atmospheres of the gastrointestinal tract. The osmotic pressure of the gastrointestinal tract is unpredictable and variable, attributed to diet, health and peristaltic mobility. Thus, a dosage form provided by this invention must develop an internal osmotic pressure greater than the osmotic pressure of the gastrointestinal tract, which, for this invention, is at least 10 atmospheres or higher in the dosage form, to provide a controlled rate of delivery of tacrine over a prolonged time. This invention effects an internal osmotic pressure of 10 atmospheres or more by blending tacrine, for example tacrine hydrochloride, with a fluid-imbibing, osmotically effective compound possessing a...

example 2

The dosage form of Example 1 is manufactured with a dose of tacrine coated on the exterior surface of the semipermeable wall. The dose of tacrine on the exterior wall comprises a pulsed dose of 15 mg of tacrine.

example 3

A dosage form adapted, designed and shaped as an osmotic tacrine dosage form is manufactured as follows: first, 3,290 g of tacrine hydrochloride and 3,290 g of mannitol are added to a Freund Flow-Coater bowl, a fluid bed granulator. The bowl is attached and the granulation process is initiated. Next, the dry materials are air suspended and mixed for 7 to 8 minutes. Then, a solution prepared by dissolving 175 g of poly(vinylpyrrolidone) having a molecular weight of 40,000 in 260 g of distilled water is sprayed onto the materials. The blending conditions are monitored during the process of spraying the aqueous poly(vinylpyrrolidone) at a solution spray rate of 125 g / min with an inlet temperature of 45.degree. C. and an air flow of 1,000 cfm. Next, the granules are blended with 35 g of hydroxypropylmethylcellulose and 210 mg of magnesium stearate and the granulation transferred to a Rotocone mixer and mixed to provide homogenous granules.

Next, a hydrogel expansion composition is prepar...

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PUM

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Abstract

A dosage form is disclosed for administering 10 ng to 1200 mg tacrine to a patient in need of tacrine therapy.

Description

This invention pertains to therapy indicated for the management of neurological diseases. More particularly, the invention relates to a dosage form that provides a controlled delivery of tacrine over an extended time for the treatment of neurological diseases, including Alzheimer's disease. The invention concerns additionally a therapeutic composition of matter comprising tacrine useful for treating neurological diseases, including Alzheimer's disease. The invention relates further to a method of administering tacrine to produce a beneficial effect for treating neurological diseases, including Alzheimer's disease.The drug tacrine is indicated for the treatment of neurological diseases, including Alzheimer's disease. The neurological-Alzheimer's disease is a progressive, irreversible brain disorder that strikes more frequently with advancing age. The common symptoms of this neurological disease generally include memory loss, confusion, impaired judgment, personality changes, and the ...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K45/00A61K9/00A61K9/20A61K9/52A61K31/47A61K47/30
CPCA61K9/0004A61K31/00A61K45/06A61K9/2018A61K9/2027A61K9/2054A61K2300/00A61K31/47A61K9/00
Inventor GUITTARD, GEORGE V.CHILDERS, JERRY D.WONG, PATRICK S.-L.GUMUCIO, FERNANDO E.KIDNEY, DAVID J.
Owner ENCINAL PHARMA INVESTMENTS
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